Development of small molecule agonists of the parathyroid hormone receptor type-1 (PTHR1) as potential new therapeutics for the treatment of osteoporosis

National Center For Advancing Translational Sciences

Investigators

Abstract

Previously, the collaborative team worked to conduct a medicinal chemistry campaign around the active PTHR1 chemotypes to explore structure-activity relationships (SAR) and improve compound potency. During this period, several lead compounds were selected for more advanced characterization, with a view to elucidating compound mechanism of action. As a center, the NCGC has fostered and maintained over 130 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to dozens of high-throughput screens and a number of medicinal chemistry campaigns to further improve on screening hits, providing our collaborators and the general research community with publications and a variety of promising small molecule probes and leads. In addition, the NCGC has worked to advance a number of informatic initiatives to make better use of existing drug and disease target information and provide the general public with easily accessible resources, further catalyzing the development of new therapies for human disease.